Titeler M, Weinreich P, Sinclair D, Seeman P
Proc Natl Acad Sci U S A. 1978 Mar;75(3):1153-6. doi: 10.1073/pnas.75.3.1153.
This study was done to obtain direct in vitro evidence for the possible existence of more than one type of dopaminergic binding site in homogenates of the caudate nucleus from calf brain. Five radioligands for dopaminergic sites were tested. The inhibitions of two agonist radioligands ([3H]dopamine, [3H]apomorphine) by haloperidol, chlorpromazine, or piflutixol were biphasic. The inhibitions of [3H]haloperidol, [3H]spiroperidol, and [3H]dihydroergocryptine binding by dopamine and (-)-norepinephrine were also biphasic. Thus, both 3H-labeled agonists and 3H-labeled antagonists were possibly binding to two high-affinity sites.
本研究旨在获取直接的体外证据,以证明小牛脑尾状核匀浆中可能存在不止一种类型的多巴胺能结合位点。测试了五种用于多巴胺能位点的放射性配体。氟哌啶醇、氯丙嗪或匹氟噻醇对两种激动剂放射性配体([³H]多巴胺、[³H]阿扑吗啡)的抑制作用呈双相性。多巴胺和(-)-去甲肾上腺素对[³H]氟哌啶醇、[³H]螺哌啶醇和[³H]二氢麦角隐亭结合的抑制作用也呈双相性。因此,³H标记的激动剂和³H标记的拮抗剂都可能与两个高亲和力位点结合。